Trials@uspto.gov
`571.272.7822
`
`
`
`
` Paper No. 13
`
` Entered: July 6, 2018
`
`
`
`
`
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`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`KVK-TECH, INC.
`Petitioner,
`
`v.
`
`SHIRE PLC
`Patent Owner.
`____________
`
`
`
`Case IPR2018-00293
`Patent 9,173,857 B2
`
`
`Before RAMA G. ELLURU, SHERIDAN K. SNEDDEN, and
`DEVON ZASTROW NEWMAN, Administrative Patent Judges.
`
`NEWMAN, Administrative Patent Judge.
`
`
`
`
`
`DECISION
`Institution of Inter Partes Review
`35 U.S.C. § 314
`
`
`
`
`
`
`
`
`571.272.7822
`
`
`
`
` Paper No. 13
`
` Entered: July 6, 2018
`
`
`
`
`
`
`
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`KVK-TECH, INC.
`Petitioner,
`
`v.
`
`SHIRE PLC
`Patent Owner.
`____________
`
`
`
`Case IPR2018-00293
`Patent 9,173,857 B2
`
`
`Before RAMA G. ELLURU, SHERIDAN K. SNEDDEN, and
`DEVON ZASTROW NEWMAN, Administrative Patent Judges.
`
`NEWMAN, Administrative Patent Judge.
`
`
`
`
`
`DECISION
`Institution of Inter Partes Review
`35 U.S.C. § 314
`
`
`
`
`
`
`
`
`
`IPR2018-00293
`Patent 9,173,857 B2
`
`
`I. INTRODUCTION
`
`KVK-Tech, Inc. (“Petitioner”) filed a corrected Petition requesting an
`
`inter partes review of claims 1–29 of U.S. Patent No. 9,173,857 B2
`
`(Ex. 1001, “the ’857 patent”). Paper 7 (“Pet.”). Shire PLC (“Patent
`
`Owner”) filed a Preliminary Response to the Petition. Paper 91 (“Prelim.
`
`Resp.”).
`
`We have authority under 35 U.S.C. § 314, which provides that an
`
`inter partes review may not be instituted “unless . . . there is a reasonable
`
`likelihood that the petitioner would prevail with respect to at least 1 of the
`
`claims challenged in the petition.” 35 U.S.C. § 314(a). On April 24, 2018,
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`the Supreme Court held that a decision to institute under 35 U.S.C. § 314
`
`may not institute on fewer than all the claims challenged in the petition. SAS
`
`Inst., Inc. v. Iancu, 138 S. Ct. 1348, 1359–60 (2018).
`
`Upon considering the Petition and Preliminary Response, we
`
`determine that Petitioner has established a reasonable likelihood that it
`
`would prevail in showing the unpatentability of at least claim 1 of the ’857
`
`patent. Accordingly, we institute an inter partes review of all challenged
`
`claims and grounds asserted in the Petition. See “Guidance on the impact of
`
`SAS on AIA trial proceedings” (April 26, 2018)
`
`(https://www.uspto.gov/patents-application-process/patent-trial-and-appeal-
`
`board/trials/guidance-impact-sas-aia-trial).
`
`
`
`1 Shire first filed a confidential version of the Patent Owner’s Preliminary
`Response. Paper 8.
`
`2
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`
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`IPR2018-00293
`Patent 9,173,857 B2
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`A. Related Proceedings
`
`Petitioner identifies a concurrently filed petition for inter partes
`
`review of claims 1–31 of the parent patent to the ’857 patent, U.S. Patent
`
`No. 8,846,100 (the “’100 patent”) based on similar grounds, which has been
`
`assigned Case No. IPR2018-00290. Pet. 3. Patent Owner asserts that the
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`’857 patent is being asserted in Shire Development LLC et al v. Teva
`
`Pharmaceuticals USA, Inc. et al, 1:17-cv-01696-RGA (D. Del). Paper 3, 1.
`
`
`
`B. The ’857 Patent
`
`The ’857 patent relates to a “long-acting amphetamine pharmaceutical
`
`composition, which includes an immediate release component, a delayed
`
`pulsed release component and a sustained release component, to meet the
`
`therapeutic needs for [Attention Deficit Hyperactivity Disorder “ADHD”]
`
`patients with longer-day demands.” Ex. 1001, 3:61–65.
`
`ADDERALL is the immediate release (“IR”) formulation of a mixture
`
`of four amphetamine salts indicated for the treatment of ADHD in children.
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`Id. at 1:59– 3:19. The ’857 patent describes multiple solutions known in the
`
`art for lengthening the release of orally consumed drugs, including
`
`ADDERALL XR, which extended the release profile of ADDERALL. Ex.
`
`1003 at 4. However, the ’857 patent indicates that some patients require an
`
`additional dosage of medication to extend the short-acting effect even
`
`further, such that “clinicians have augmented the morning long-acting
`
`formulation, typically at 8-10 hours post-dose [of ADDERALL XR], with a
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`dose of the same immediate-release (IR) medication.” Id. at 3:42–51.
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`Consequently, the ’857 patent states that a need exists for a “once-daily,
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`long-acting oral composition that provides effective treatment of ADHD,
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`3
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`IPR2018-00293
`Patent 9,173,857 B2
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`without supplementation, for patients with longer day demands (e.g., 14-16
`
`awake hours).” Id. at 3:54–57.
`
`The disclosed long-acting amphetamine pharmaceutical composition
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`includes “an immediate release component, a delayed pulsed release
`
`component and a sustained release component, to meet the therapeutic needs
`
`for ADHD patients with longer-day demands.” Id. at 3:61–65. The ’857
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`patent states that the composition is “bioequivalent to an equal dosage of
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`ADDERALL XR® followed by an IR amphetamine composition 8 hours
`
`later.” Id. at 3:65–43; 4:9–11.
`
`
`
`C. Illustrative Claim
`
`Petitioner challenges claims 1–29 of the ’857 patent, of which claim 1
`
`is the only independent claim. Claim 1 is representative and is reproduced
`
`below:
`
`1. A method for treating attention deficit hyperactivity disorder
`(ADHD) which comprises:
`
`administering to a patient in need thereof, a pharmaceutical
`composition comprising:
`
`(a) an immediate release bead comprising at least one amphetamine
`salt;
`(b) a first delayed release bead comprising at least one
`amphetamine salt; and
`(c) a second delayed release bead comprising at least one
`amphetamine salt; wherein the first delayed release bead
`provides pulsed release of the at least one amphetamine salt and
`the second delayed release bead provides sustained release of
`the at least one amphetamine salt;
`
`wherein the second delayed release bead comprises at least one
`amphetamine salt layered onto or incorporated into a core; a
`delayed release coating layered onto the amphetamine core; and
`a sustained release coating layered onto the delayed release
`coating,
`
`4
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`IPR2018-00293
`Patent 9,173,857 B2
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`wherein the sustained release coating is pH-independent; and
`wherein the first delayed release bead and the second delayed
`release bead comprise an enteric coating.
`
`
`
`D. The Asserted Grounds of Unpatentability
`
`Petitioner challenges the patentability of claims 1–29 of the
`
`’857 patent on the following grounds:
`
`Basis
`
`Claims challenged
`
`§ 102(a)
`
`1–19, 29
`
`Reference(s)
`
`Burnside2
`
`Burnside
`
`Adderall XR3,4 and Burnside
`
`§ 103
`
`§ 103
`
`1–29
`
`1–29
`
`Petitioner also relies on the following declarations:
`
`Exhibit
`
`Reference
`
`1004
`
`Declaration of Diane J. Burgess, Ph.D.
`
`1006
`
`Declaration of William J. Jusko, Ph.D.
`
`II. ANALYSIS
`
`A. Discretionary Denial
`
`35 U.S.C. § 325(d) provides, in relevant part: “In determining whether
`
`to institute or order a proceeding under this chapter, chapter 30, or chapter
`
`31, the Director may take into account whether, and reject the petition or
`
`
`
`2 Burnside, Beth A. et al., US 6,605,300 B1, issued August 12, 2003
`(“Burnside,” Ex. 1002).
`3 PHYSICIANS’ DESK REFERENCE, entry for Adderall XR, 3144–3146
`(58th ed. 2004) (“ADDERALL XR,” Ex. 1003).
`4 FDA ADDERALL XR Label, 2004 (Published August 2004)
`(“ADDERALL XR,” Ex. 1031).
`
`5
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`IPR2018-00293
`Patent 9,173,857 B2
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`request because, the same or substantially the same prior art or arguments
`
`previously were presented to the Office.” See Unified Patents, Inc. v.
`
`Berman, Paper 10, No. IPR2016-01571 (14 December 2016) (informative),
`
`Hospira, Inc. v. Genentech, Inc., Paper 16, No. IPR2017-00739 (27 July
`
`2017) (informative); and Cultec, Inc. v. Stormtech LLC, Paper 7, No.
`
`IPR2017-00777 (22 August 2017) (informative).
`
`Patent Owner argues that the Board should exercise discretion under
`
`35 U.S.C. § 325(d) to deny the Petition because both Burnside and
`
`ADDERALL XR were before the Examiner during prosecution of the ’857
`
`patent. Prelim. Resp. 4–8. In support, Patent Owner asserts that Petitioner’s
`
`“arguments in Grounds 1 and 2, regarding anticipation or obviousness based
`
`on Burnside, are identical to those raised and considered by the Examiner
`
`and ultimately overcome by Applicants” and that the Petition is substantially
`
`based on “prior art and arguments” presented during prosecution. Id. at 4.
`
`Petitioner argues against discretionary denial, asserting that although
`
`“some of the same prior art relied upon in the Grounds was before the Patent
`
`Office during prosecution of the ‘100 [parent patent] and ‘857 patents,” the
`
`Petition presents “new additional prior art and arguments not previously
`
`presented.” Pet. 2, 63–65. Of particular relevance to our discretionary
`
`denial,5 Petitioner argues that “the Examiner’s amendment leading to
`
`allowance reveals that the Examiner was unaware of prior art teaching that
`
`SURELEASE® is pH independent.” Id. at 64.
`
`
`
`5 Petitioner raises additional arguments supporting its position that we should
`decline to exercise our discretion under § 325(d). We do not address those
`herein as we are persuaded that the sole issue discussed is sufficient to
`justify our decision to decline to exercise our discretion under § 325(d).
`
`6
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`IPR2018-00293
`Patent 9,173,857 B2
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`Based on the facts of this record, we decline to exercise our discretion
`
`under § 325(d) to deny the instant petition because the current record
`
`presents arguments and evidence not considered by the Examiner. During
`
`prosecution of the ’100 patent (the parent of the ’857), the Examiner
`
`considered Burnside and ADDERALL XR. See, e.g., Ex. 1005, 482–84,
`
`553, 667. The Examiner also was aware that the prior art disclosed polymer
`
`outer coatings of drugs, including Burnside’s disclosure of outer
`
`coatings. Ex. 1005, 483–84. The Examiner subsequently entered an
`
`amendment to independent claim 1, the sole independent claim, which led to
`
`its allowance. Id. at 785–86, 808. The amendment recites “wherein the
`
`sustained release coating is pH-independent.” Id. at 785. The Examiner-
`
`Initiated Interview Summary notes “Applicant presented arguments to
`
`distinguish the instant invention over the prior art. Examiner suggested
`
`amending the claims to further distinguish over the prior art which requires
`
`pH dependent polymers in the outer coating. Applicant agreed to consider
`
`the amendment.” Id. at 787. No other amendments were entered. The
`
`current record, however, includes evidence not considered by the Examiner
`
`showing that the prior art the Examiner considered disclosed a pH-
`
`independent coating material, namely SURELEASE.
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`Burnside discloses the use of SURELEASE as a “protective coating
`
`layer” for drug formulations. Ex. 1002 8:17–30. To support its argument
`
`that SURELEASE is pH-independent, Petitioner relies on new information
`
`from prior art references, not in the record before the Examiner, submitted
`
`here as Exhibits 1007, 1034, and 1035. Pet. 25–27. According to Petitioner,
`
`these exhibits “expressly state SURELEASE® is pH-independent and
`
`identify SURELEASE® as ethylcellulose, which was known to be pH
`
`7
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`IPR2018-00293
`Patent 9,173,857 B2
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`independent.” Id.; see Ex. 1004 ¶¶ 74–77; Ex. 1007, 5; Ex. 1034, 13:11–12;
`
`Ex. 1035, 11:18–25.
`
`We decline to exercise our discretion under § 325(d) to deny the
`
`petition for the following reasons.
`
`With regard to the issue of whether the Examiner was aware that
`
`SURELEASE is pH-independent ethylcellulose, Patent Owner argues that
`
`the “prosecution [history] does not support [Petitioner’s] argument that the
`
`Examiner was unaware of the pH properties of a SURELEASE polymer
`
`coating” because the Examiner “referred to ‘SURELEASE®, an
`
`ethylcellulose compound,’” “Applicants identified ethylcellulose as ‘a water
`
`insoluble polymer,’” the “[S]pecification disclosed a ‘low water-permeable
`
`pH-insensitive polymer’ for over-coating the SR bead, and exemplified
`
`SURELEASE® (ethylcellulose),” and “the Amendment confronted pH-
`
`dependent components in outer coatings of Percel, not Burnside.” Prelim.
`
`Resp. 7.
`
`We agree with Patent Owner that the record indicates that the
`
`Examiner was aware that SURELEASE is an ethylcellulose compound. Ex.
`
`1005, 702. However, the record does not indicate that the Examiner was
`
`aware that SURELEASE is pH-independent. As noted above, Burnside
`
`Example 4, which was used as one basis of the rejection at issue,
`
`exemplified SURELEASE as a sustained-release coating. Ex. 1002, 11:59–
`
`12:26. The Examiner suggested “amending the claims to further distinguish
`
`over the prior art which requires pH dependent polymers in the outer
`
`[sustained release] coating.” Ex. 1005, 787. The limitation “wherein the
`
`sustained release coating is pH-independent” was subsequently added by
`
`Examiner’s amendment. Id. at 785–787. Thus, based on the current record,
`
`we determine the Examiner was unaware that SURELEASE is pH-
`
`8
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`IPR2018-00293
`Patent 9,173,857 B2
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`independent at the time the amendment was suggested and entered. That the
`
`Specification exemplifies SURELEASE as a “‘low water-permeable pH-
`
`insensitive polymer’ for over-coating the SR [sustained release] bead,” is not
`
`dispositive of the Examiner’s understanding given the clear wording of the
`
`Examiner’s suggested amendment.
`
`The arguments, and supporting evidence, in this proceeding, therefore,
`
`are significantly different than those asserted during prosecution. Here,
`
`Petitioner’s argument that SURELEASE is pH-independent, and Petitioner’s
`
`supporting evidence, were not considered by the Examiner. Accordingly,
`
`we decline to exercise our discretion under § 325(d) given the difference in
`
`arguments and evidence in this case.
`
`B. Person of Ordinary Skill in the Art
`
`Petitioner asserts that a person of ordinary skill in the art would have
`
`had “at least a Bachelor of Science Degree in Pharmacy, Chemistry, or
`
`Chemical Engineering, or similar field, and experience in the field of
`
`pharmaceutics (including pharmaceutical formulation or pharmacokinetics
`
`or a similar technical field of study).” Pet. 16; Ex. 1004 ¶ 21. Petitioner
`
`further asserts that a person of ordinary skill in the art would have had
`
`“access to and may consult with a pharmacologist with experience in
`
`pharmacokinetics and/or an M.D. with experience with ADHD and
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`pharmacological treatments for ADHD.” Id.
`
`Patent Owner asserts that a person of ordinary skill in the art at the
`
`time of the invention would have had “a Bachelor of Science Degree in
`
`Pharmacy, Chemistry, or Chemical Engineering, or similar field, and three
`
`years of experience in the field of pharmaceutics (including pharmaceutical
`
`9
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`IPR2018-00293
`Patent 9,173,857 B2
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`formulation or pharmacokinetics or a similar technical field of study).”
`
`Prelim. Resp. 13; Ex. 20016 ¶ 22.
`
`We do not discern an appreciable difference in the parties’ respective
`
`definitions of the level of ordinary skill in the art. Both parties contend that
`
`a person of ordinary skill in the art would have had similar education levels
`
`and experience with and knowledge of the development of pharmaceutical
`
`formulations and the ability to analyze pharmacokinetic data. Thus, on this
`
`record, we determine it is unnecessary to resolve any perceived differences
`
`in the parties’ definitions of the level of ordinary skill in the art, as any
`
`distinction does not impact our Decision. We further note that, in this case,
`
`the prior art itself demonstrates the level of skill in the art at the time of the
`
`invention. See Okajima v. Bourdeau, 261 F.3d 1350, 1355 (Fed. Cir. 2001)
`
`(explaining that specific findings regarding ordinary skill level are not
`
`required “where the prior art itself reflects an appropriate level and a need
`
`for testimony is not shown”) (quoting Litton Indus. Prods., Inc. v. Solid
`
`State Sys. Corp., 755 F.2d 158, 163 (Fed. Cir. 1985)).
`
`
`
`C. Claim Construction
`
`In an inter partes review, the Board interprets claim terms in an
`
`unexpired patent according to the broadest reasonable construction in light
`
`of the specification7 of the patent in which they appear. 37 C.F.R. § 100(b);
`
`Cuozzo Speed Techs., LLC v. Lee, 136 S. Ct. 2131, 2142 (2016) (affirming
`
`applicability of broadest reasonable construction standard to inter partes
`
`
`
`6 Patent Owner relies on the Declaration of Bernhardt L. Trout, Ph.D.,
`hereinafter “Trout Dec.”). Ex. 2001.
`7 References to the Specification herein refer to the specification of the
`parent ’100 patent.
`
`10
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`IPR2018-00293
`Patent 9,173,857 B2
`
`review proceedings). Under that standard, and absent any special
`
`definitions, we generally give claim terms their ordinary and customary
`
`meaning, as would be understood by one of ordinary skill in the art at the
`
`time of the invention. See In re Translogic Tech., Inc., 504 F.3d 1249, 1257
`
`(Fed. Cir. 2007). Any special definitions for claim terms must be set forth
`
`with reasonable clarity, deliberateness, and precision. See In re Paulsen, 30
`
`F.3d 1475, 1480 (Fed. Cir. 1994).
`
`1.
`
`“about”
`
`The term “about” appears in multiple dependent claims. Ex. 1001,
`
`32:45–34:21. Each party argues that the Specification supports its
`
`interpretation of “about.” Petitioner argues that “‘about’ can mean a range
`
`of up to 20% . . . of a given value.” Pet. 17 (citing Ex. 1001, 12:18–20).
`
`Patent Owner argues that “about” means “approximately.” Prelim. Resp.
`
`(citing Ex. 1001, 12:10).
`
`The claim term “about” appears in dependent claims 5–12 and 22–30.
`
`For example, claim 5 recites “wherein administration of a 37.5 mg dose of
`
`the pharmaceutical composition to a human patient results in a d-
`
`amphetamine Cm ax of about 50 ng/ml” and claim 22 recites “wherein the
`
`amount of at least one amphetamine salt is about 12.5 mg.” Petitioner
`
`argues that the term “about” should be construed consistent with its broadest
`
`reasonable interpretation. Pet. 16. According to Petitioner, “about” can
`
`mean “a range of up to 20% . . . of a given value.” Id. (citing Ex. 1001,
`
`11:61–64; 11:65–12:6). Patent Owner argues that “about” is defined by the
`
`Specification in accordance with the term’s ordinary meaning,
`
`“approximately.” Prelim. Resp. 19 (citing Ex. 1001, 11:65–12:4; Pet. 16).
`
`The ’857 patent defines “about” as follows:
`
`11
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`
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`IPR2018-00293
`Patent 9,173,857 B2
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`The term “about” or “approximately” means within an
`acceptable error range for the particular value as determined by
`one of ordinary skill in the art, which will depend in part on how
`the value is measured or determined, i.e., the limitations of the
`measurement system, i.e., the degree of precision required for a
`particular purpose, such as a pharmaceutical formulation. For
`example, “about” can mean within 1 or more than 1 standard
`deviations, per the practice in the art. Alternatively, “about” can
`mean a range of up to 20%, preferably up to 10%, more
`preferably up to 5%, and more preferably still up to 1% of a given
`value. Alternatively, particularly with respect to biological
`systems or processes, the term can mean within an order of
`magnitude, preferably within 5-fold, and more preferably within
`2-fold, of a value.
`
`Ex. 1001, 11:65–12:11.
`
`We construe “about” precisely as defined by the Specification, which
`
`encompasses each of the above, three, listed examples.
`
`2.
`
`No “food effect”
`
`The claim term “food effect” appears in challenged dependent claim
`
`19, which recites “wherein the composition does not exhibit a food effect.”
`
`Ex. 1001, 34:1–2. Petitioner argues that this claim term should be construed
`
`consistent with its broadest reasonable interpretation and refers to the ’100
`
`patent specification’s definition of “food effect.” Pet. 17 (citing Ex. 1001,
`
`11:61–64). Patent Owner contends that the specification “expressly defines”
`
`this term in connection with “‘bioavailability,’” and not “‘absorption.’”
`
`Prelim. Resp. 20 (citing Ex. 1004, ¶¶ 57–58; Pet. 16).
`
`The ’857 patent specification defines “food effect” as “a significant
`
`difference in the bioavailability of a drug in a patient when the drug is
`
`administered in a fasted state compared to a fed state.” Ex. 1001, 12:4–9.
`
`Thus, we construe no “food effect” precisely as defined by the
`
`specification—no “significant difference in the bioavailability of a drug in a
`
`12
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`IPR2018-00293
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`patient when the drug is administered in a fasted state compared to a fed
`
`state.”
`
`D. Obviousness over ADDERALL XR and
`
`Burnside
`
`Petitioner asserts that claims 1–29 of the ’857 patent are obvious
`
`under 35 U.S.C. § 103(a) over ADDERALL XR and Burnside. Pet. 5, 35–
`
`61. Patent Owner opposes Petitioner’s assertion. Prelim. Resp. 2–8, 43–46,
`
`56–65. On this record, we determine that Petitioner has established a
`
`reasonable likelihood that it would prevail in showing that at least claim 1 is
`
`obvious over these references.
`
`1.
`
`ADDERALL XR (Ex. 1003, 1031)
`
`ADDERALL XR is a once daily extended-release, single-entity
`
`amphetamine product with a methacrylic acid copolymer enteric coating.
`
`Ex. 1031, 1. ADDERALL XR is indicated for the treatment of Attention
`
`Deficit Hyperactivity Disorder (ADHD). Id. at 3.
`
`ADDERALL XR is administered as a capsule containing “two types
`
`of drug-containing beads designed to give a double-pulsed delivery of
`
`amphetamines, which prolongs the release of amphetamine” as compared to
`
`ADDERALL IR formulation.8 Ex. 1031, 5. In addition, food does not affect
`
`the extent of absorption of ADDERALL XR. Id. at 2.
`
`
`
`8 Patent Owner’s declarant explains that ADDERALL XR comprises the
`same amphetamine salts as Adderall IR “within immediate release beads and
`delayed pulsed beads with an enteric coating.” Ex. 1004 ¶ 32.
`
`13
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`IPR2018-00293
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`2.
`
`Burnside (Ex. 1002)
`
`Burnside relates to a multiple unit dosage form delivery system
`
`comprising one or more amphetamine salts for administering the
`
`amphetamine salts to a recipient. Ex. 1002 at 1:9–11.
`
`Burnside discloses examples in which amphetamine salts are layered
`
`onto sugar spheres for drug delivery. Id. at 10:60–12:26. Burnside also
`
`provides examples in which the amphetamine salts are further coated with a
`
`“protective layer” (enteric coating) to delay the drug release. Id. at 10:59–
`
`12:26. Burnside discloses that “suitable materials for the protective layer
`
`include cellulose derivatives such as hydroxyethyl cellulose, hydroxypropyl
`
`cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone,
`
`polyvinylpyrrolidone/vinyl acetate copolymer, ethyl cellulose aqueous
`
`dispersions (AQUACOAT ®, SURELEASE®), EUDRAGIT ® RL 30D,
`
`OPADRY® and the like.” Id. at 8:20–29. Example 2 of Burnside discloses
`
`the coating of mixed amphetamine salts with EUDRAGIT L. Id. at 10:60–
`
`11:8. “[T]he enteric coating delayed the drug release from the coated pellets
`
`until after exposure to pH 6 or higher.” Id. at 11:9–10. Figure 4 of Burnside
`
`is depicted below:
`
`
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`14
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`IPR2018-00293
`Patent 9,173,857 B2
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`Figure 4 illustrates the drug release profile of the coated pellets in Example
`
`2. Id. at 11:23–24.
`
`Example 3 discloses coating of mixed amphetamine salts with
`
`EUDRAGIT 4110D. Id. at 11:26–11:41. “[T]he enteric coating delayed the
`
`drug release from the coated pellets until the pH value reached 6.8 or
`
`higher.” Id. at 11:41–43. Figure 5 of Burnside is depicted below:
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`
`
`
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`Figure 5 illustrates the drug release profile of the coated pellets in Example
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`3. Id. at 11:56–57.
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`Example 4 discloses applying an additional coating to the coated
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`pellets from Example 2 or Example 3 by spraying SURELEASE coating on
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`the outer surfaces of the coated pellets. Id. at 11:59–12:9. Burnside states
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`that “the SURELEASE® coating slightly sustained the drug release from
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`EUDRAGIT ® L 30D-55 coated pellets at pH 7.5 buffer, while the
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`SURELEASE® coating delayed the drug release up to 2 hours after the
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`buffer switched from pH 1 to pH 7.5.” Id. at 12:9–14. Figure 6 of Burnside
`
`is depicted below:
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`15
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`IPR2018-00293
`Patent 9,173,857 B2
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`
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`
`
`Figure 6 illustrates the drug release profile of the coated pellets in Example
`
`4. Id. at 12:25–26.
`
`Example 5 of Burnside discloses a “pulsatile delivery system”
`
`achieved by combining the IR pellets of Example 1 with the delayed release
`
`pellets of Example 2 or Example 3. Id. at 12:29–31. Burnside discloses that
`
`pellets of both types equivalent to half of the total dose are “filled into a hard
`
`gelatin capsule to produce the oral pulsed dose delivery system. The
`
`delayed-release portion releases the amphetamine salts rapidly and
`
`completely, after a specified lag time.” Id. at 12:31–36. Figure 8 of
`
`Burnside is depicted below:
`
`16
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`IPR2018-00293
`Patent 9,173,857 B2
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`
`
`
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`Figure 8 is the drug release profile of the coated pellets in Example 5. Id. at
`
`12:40–41.
`
`3.
`
`Analysis
`
`A claim is unpatentable under 35 U.S.C. § 103(a) if the differences
`
`between the claimed subject matter and the prior art are such that the subject
`
`matter, as a whole, would have been obvious at the time the invention was
`
`made to a person having ordinary skill in the art to which the subject matter
`
`pertains. KSR Int’l Co. v. Teleflex Inc., 550 U.S. 398, 406 (2007). The
`
`question of obviousness is resolved on the basis of underlying factual
`
`determinations, including: (1) the scope and content of the prior art; (2) any
`
`differences between the claimed subject matter and the prior art; (3) the level
`
`of skill in the art; and (4) objective evidence of nonobviousness. Graham v.
`
`John Deere Co., 383 U.S. 1, 17–18 (1966).
`
`“[A] patent composed of several elements is not proved obvious
`
`merely by demonstrating that each of its elements was, independently,
`
`17
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`IPR2018-00293
`Patent 9,173,857 B2
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`known in the prior art.” KSR, 550 U.S. at 418. “[I]t can be important to
`
`identify a reason that would have prompted a person of ordinary skill in the
`
`relevant field to combine elements in the way the claimed new invention
`
`does.” Id. Moreover, a person of ordinary skill in the art must have had a
`
`reasonable expectation of success in doing so. PAR Pharm., Inc. v. TWi
`
`Pharms., Inc., 773 F.3d 1186, 1193 (Fed. Cir. 2014).
`
`Petitioner asserts that claims 1–29 would have been obvious over the
`
`combination of Adderall XR and Burnside. Pet. 5, 39–52. Petitioner
`
`provides detailed claim charts mapping disclosure from the combined
`
`teachings of ADDERALL XR and Burnside to the limitations of the
`
`challenged claims. Pet. 39–51. After considering the evidence and
`
`arguments presented in the Petition and Preliminary Response, we determine
`
`that Petitioner has demonstrated a reasonable likelihood of prevailingin
`
`proving that at least claim 1 of the ’857 patent is unpatentable over the
`
`combination of ADDERALL XR and Burnside.
`
`4.
`
`Claim 1
`
`Claim 1 recites a method for treating ADHD comprising
`
`administering a pharmaceutical composition comprising: (1) an immediate
`
`release bead (“IR bead”) comprising at least one amphetamine salt; (2) a
`
`first delayed release bead (“first DR bead”) comprising at least one
`
`amphetamine salt, wherein the first DR bead provides a pulsed release of the
`
`amphetamine salt, and wherein the first DR bead comprises an enteric
`
`coating; and (3) a second delayed release bead (“second DR bead”)
`
`comprising at least one amphetamine salt, wherein the second DR bead
`
`provides sustained release of the amphetamine salt, comprises at least one
`
`amphetamine salt layered onto or incorporated into a core, a delayed release
`
`coating layered onto the core, and a sustained release coating layered onto
`
`18
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`
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`IPR2018-00293
`Patent 9,173,857 B2
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`the delayed release coating, wherein the sustained release coating is pH-
`
`independent, and wherein the second DR bead comprises an enteric coating.
`
`Thus, the claimed composition comprises three types of beads, each of
`
`which contains a core of amphetamine salt. The first DR bead provides a
`
`pulsed release of the salt and comprises an enteric coating. The second DR
`
`bead provides a sustained release of the salt, comprises a delayed release
`
`coating layered onto the core, and a sustained release coating layered onto
`
`the delayed release coating, wherein the sustained release coating is pH-
`
`independent and wherein the second DR bead also comprises an enteric
`
`coating.
`
`With respect to the claimed IR bead, Petitioner refers to each of
`
`ADDERALL XR and Burnside. Pet. 40 (citations omitted). Petitioner notes
`
`that the plasma concentration of ADDERALL XR is comparable to two
`
`divided doses of ADDERALL IR doses administered four hours apart twice
`
`a day. Id. Petitioner also refers to Burnside’s Example 1 as teaching the
`
`claimed IR bead. Id. at 25 (citing Ex. 1004, ¶¶ 63–64).
`
`With respect to the first DR bead, Petitioner refers to each of
`
`ADDERALL XR and Burnside. Petitioner argues that ADDERALL XR
`
`expressly or inherently teaches the claimed first DR bead. Id. at 44.
`
`According to Petitioner, plasma concentration graphs comparing the
`
`independent doses of ADDERALL IR and ADDERALL XR confirm that
`
`the second pulsed delivery of ADDERALL XR is the result of the delayed
`
`release beads. Id. Further, asserts Petitioner, the delayed release beads of
`
`ADDERALL XR include an enteric coating. Id. at 45 (citing Ex. 1004, ¶
`
`145). Petitioner also refers to Burnside’s Examples 2 and 3 as teaching the
`
`19
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`IPR2018-00293
`Patent 9,173,857 B2
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`claimed first DR bead. Id. at 20–21 (citations omitted); id at 25 (citing Ex.
`
`1004 ¶¶ 63–64).9
`
`With respect to the second DR bead, Petitioner refers to Burnside.
`
`Specifically, Petitioner argues that Burnside’s Example 4 discloses “the
`
`claimed sustained release beads, comprising at least one amphetamine salt
`
`on a core, a delayed release (enteric) coating on the amphetamine salt and a
`
`sustained release (SURELEASE®) coating over the delayed (enteric) release
`
`coating.” Id. at 25 (citing Ex. 1004 ¶¶ 46–50, 70–77). Petitioner further
`
`contends that a skilled artisan would have known that SURELEASE is a
`
`sustained release coating that is pH-independent. Id. at 25–26.
`
`Petitioner argues that a skilled artisan would have been motivated “to
`
`prolong the therapeutic efficacy provided by the two-bead systems of
`
`Example 5 of Burnside and/or Adderall XR®.” Id. at 52. Petitioner avers
`
`that it was known that ADDERALL XR was inadequate for a certain
`
`proportion of patients who would “benefit from a composition that prolongs
`
`the release of the amphetamine actives longer than Adderall XR®.” Id. at
`
`52–53. To address this problem, the prior art taught administering a second
`
`ADDERALL IR dose, and thus, a skilled artisan would have had reason to
`
`create a “once-daily” composition “to meet the demand for a longer duration
`
`of efficacy than provided by Adderall XR®.” Id. at 53. Petitioner contends
`
`that to do so, a skilled artisan would have added “the sustained release beads
`
`taught by Example 4 of Burnside to Example 5 of Burnside and/or Adderall
`
`XR®.” Id. citing (Ex. 1004 ¶¶ 39, 158–169). Petitioner further cites
`
`
`
`9 Petitioner notes that during prosecution, Patent Owner admitted that
`Burnside discloses delayed pulse release beads. Id. at 25 (citing Ex. 1004 ¶¶
`78–79; Ex. 1005, 569).
`
`20
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`IPR2018-00293
`Patent 9,173,857 B2
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`Exhibits 1015, 1023, and 1038 as additional “motivational” references that
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`would have motivated a skilled artisan to make the claimed combination.
`
`Pet. 52–56.
`
`Patent Owner disagrees that the combination of ADDERALL XR and
`
`Burnside would have rendered claims 1–29 obvious. Patent Owner initially
`
`argues that Burnside does not disclose the claimed three bead composition.
`
`Prelim. Resp. 53–54. Specifically, Patent Owner contends that Burnside is
`
`“missing” (emphasis omitted) the claimed “second delayed release bead”
`
`with a pH-independent “sustained release coating layered onto the delayed
`
`coating.” Id. at 48. Patent Owner further argues that there was no
`
`suggestion to combine such a bead with immediate release beads and
`
`delayed release beads because there was no “hint” to exploit Burnside’s
`
`Example 4. Id. In addition, Patent Owner asserts that a skilled artisan
`
`would not have been able to predict the drug release of the proposed
`
`combination. Id. at 48–49. Relying on pharmacokinetic profiles, Patent
`
`Owner further distinguishes the claimed composition that includes sustained
`
`release of amphetamine from the prior art teaching of ADDERALL XR
`
`followed by an IR pulsating dosing scheme. Id. at 49–50; id. at 51 (ass
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